葡萄糖修饰的载胰岛素脂质体以包封率为指标的制备工艺研究

目的基于乙醇对脂质双分子层膜的去稳定作用制备得较高包封率的载胰岛素脂质体。方法本研究以空白大单室脂质体在乙醇存在的条件下对胰岛素进行主动载药。考察了脂质处方、乙醇浓度、孵育温度、孵育时间、PEG2000-succ-Chol用量、药脂比等对包封率的影响。结果乙醇存在条件下空白大单室脂质体对胰岛素进行主动载药而得粒径（180±70）nm的小多室脂质体,包封率为28%～32%。结论该方法制备所得的胰岛素脂质体比文献报道的包封率提高了近2倍,而且避免了使用有机溶剂,最大程度保护了胰岛素的生物活性。

Preparation of Glucosylated Liposomes With High Encapsulation Efficiency of Insulin

Objective To prepare insulin liposmes with high encapsulation efficiency by ethanol destabilized metho.Methods In the presence of ethanol,insulin was positively encapsulated in large unilamellar vesicles.The effect of composition of phospholipid,ethanol concentration,incubation temperature,incubation time,and the presence of PEG2000-succ-Chol on the encapsulation efficiency of insulin was investigated.Results The interaction of large unilamellar vesicles with insulin leads to the formation of small multilamellar liposomes the size of（180±70）nm,and the encapsulation efficiency achieved 28%-32%.Conclusion The present method could achieve 2 fold higher entrapment efficiency than methods reported in literature.Toxic solvents are avoided to maintain the maximum bioactivity of insulin.